Bioorganic and Medicinal Chemistry Letters p. 715 - 720 (1998)
Update date:2022-09-26
Topics:
Rodgers, James D.
Johnson, Barry L.
Wang, Haisheng
Erickson-Viitanen, Susan
Klabe, Ronald M.
Bacheler, Lee
Cordova, Beverly C.
Chang, Chong-Hwan
Cyclic ureas containing 3-aminoindazole P2/P2' groups are extremely potent inhibitors of HIV protease. The parent 3-aminoindazole 6 showed a K(i) < 0.01 nM but poor translation of enzyme activity to antiviral activity was observed. A series of 3-alkylaminoindazoles revealed that translation improved with increasing lipophilicity. An X-ray crystal structure of 6 bound to HIV protease was obtained.
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Doi:10.1021/jm980061w
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(1998)
